1.Not Available.
Weile YE ; Jiaojiao WANG ; Peter J LITTLE ; Jiami ZOU ; Zhihua ZHENG ; Jing LU ; Yanjun YIN ; Hao LIU ; Dongmei ZHANG ; Peiqing LIU ; Suowen XU ; Wencai YE ; Zhiping LIU
Acta Pharmaceutica Sinica B 2024;14(1):1-19
Bioactive compounds derived from herbal medicinal plants modulate various therapeutic targets and signaling pathways associated with cardiovascular diseases (CVDs), the world's primary cause of death. Ginkgo biloba, a well-known traditional Chinese medicine with notable cardiovascular actions, has been used as a cardio- and cerebrovascular therapeutic drug and nutraceutical in Asian countries for centuries. Preclinical studies have shown that ginkgolide B, a bioactive component in Ginkgo biloba, can ameliorate atherosclerosis in cultured vascular cells and disease models. Of clinical relevance, several clinical trials are ongoing or being completed to examine the efficacy and safety of ginkgolide B-related drug preparations in the prevention of cerebrovascular diseases, such as ischemia stroke. Here, we present a comprehensive review of the pharmacological activities, pharmacokinetic characteristics, and mechanisms of action of ginkgolide B in atherosclerosis prevention and therapy. We highlight new molecular targets of ginkgolide B, including nicotinamide adenine dinucleotide phosphate oxidases (NADPH oxidase), lectin-like oxidized LDL receptor-1 (LOX-1), sirtuin 1 (SIRT1), platelet-activating factor (PAF), proprotein convertase subtilisin/kexin type 9 (PCSK9) and others. Finally, we provide an overview and discussion of the therapeutic potential of ginkgolide B and highlight the future perspective of developing ginkgolide B as an effective therapeutic agent for treating atherosclerosis.
2.Targeting FAPα-positive lymph node metastatic tumor cells suppresses colorectal cancer metastasis.
Shuran FAN ; Ming QI ; Qi QI ; Qun MIAO ; Lijuan DENG ; Jinghua PAN ; Shenghui QIU ; Jiashuai HE ; Maohua HUANG ; Xiaobo LI ; Jie HUANG ; Jiapeng LIN ; Wenyu LYU ; Weiqing DENG ; Yingyin HE ; Xuesong LIU ; Lvfen GAO ; Dongmei ZHANG ; Wencai YE ; Minfeng CHEN
Acta Pharmaceutica Sinica B 2024;14(2):682-697
Lymphatic metastasis is the main metastatic route for colorectal cancer, which increases the risk of cancer recurrence and distant metastasis. The properties of the lymph node metastatic colorectal cancer (LNM-CRC) cells are poorly understood, and effective therapies are still lacking. Here, we found that hypoxia-induced fibroblast activation protein alpha (FAPα) expression in LNM-CRC cells. Gain- or loss-function experiments demonstrated that FAPα enhanced tumor cell migration, invasion, epithelial-mesenchymal transition, stemness, and lymphangiogenesis via activation of the STAT3 pathway. In addition, FAPα in tumor cells induced extracellular matrix remodeling and established an immunosuppressive environment via recruiting regulatory T cells, to promote colorectal cancer lymph node metastasis (CRCLNM). Z-GP-DAVLBH, a FAPα-activated prodrug, inhibited CRCLNM by targeting FAPα-positive LNM-CRC cells. Our study highlights the role of FAPα in tumor cells in CRCLNM and provides a potential therapeutic target and promising strategy for CRCLNM.
3.Erratum: Author correction to "The FAPα-activated prodrug Z-GP-DAVLBH inhibits the growth and pulmonary metastasis of osteosarcoma cells by suppressing the AXL pathway" Acta Pharm Sin B 12 (2022) 1288-1304.
Geni YE ; Maohua HUANG ; Yong LI ; Jie OUYANG ; Minfeng CHEN ; Qing WENG ; Xiaobo LI ; Huhu ZENG ; Pei LONG ; Zepei FAN ; Junqiang YIN ; Wencai YE ; Dongmei ZHANG
Acta Pharmaceutica Sinica B 2023;13(3):1337-1339
[This corrects the article DOI: 10.1016/j.apsb.2021.08.015.].
4.The FAP α -activated prodrug Z-GP-DAVLBH inhibits the growth and pulmonary metastasis of osteosarcoma cells by suppressing the AXL pathway.
Geni YE ; Maohua HUANG ; Yong LI ; Jie OUYANG ; Minfeng CHEN ; Qing WEN ; Xiaobo LI ; Huhu ZENG ; Pei LONG ; Zepei FAN ; Junqiang YIN ; Wencai YE ; Dongmei ZHANG
Acta Pharmaceutica Sinica B 2022;12(3):1288-1304
Osteosarcoma is a kind of bone tumor with highly proliferative and invasive properties, a high incidence of pulmonary metastasis and a poor prognosis. Chemotherapy is the mainstay of treatment for osteosarcoma. Currently, there are no molecular targeted drugs approved for osteosarcoma treatment, particularly effective drugs for osteosarcoma with pulmonary metastases. It has been reported that fibroblast activation protein alpha (FAPα) is upregulated in osteosarcoma and critically associated with osteosarcoma progression and metastasis, demonstrating that FAPα-targeted agents might be a promising therapeutic strategy for osteosarcoma. In the present study, we reported that the FAPα-activated vinblastine prodrug Z-GP-DAVLBH exhibited potent antitumor activities against FAPα-positive osteosarcoma cells in vitro and in vivo. Z-GP-DAVLBH inhibited the growth and induced the apoptosis of osteosarcoma cells. Importantly, it also decreased the migration and invasion capacities and reversed epithelial-mesenchymal transition (EMT) of osteosarcoma cells in vitro and suppressed pulmonary metastasis of osteosarcoma xenografts in vivo. Mechanistically, Z-GP-DAVLBH suppressed the AXL/AKT/GSK-3β/β-catenin pathway, leading to inhibition of the growth and metastatic spread of osteosarcoma cells. These findings demonstrate that Z-GP-DAVLBH is a promising agent for the treatment of FAPα-positive osteosarcoma, particularly osteosarcoma with pulmonary metastases.
5.Chemical constituents of petroleum ether extract from the stems and leaves of Humulus scandens
Biao SUN ; Yunlin AO ; Dezhi WANG ; Junya WANG ; Wencai YE ; Xiaoqi ZHANG
Journal of China Pharmaceutical University 2022;53(2):178-184
To study the chemical constituents of petroleum ether extract from the stems and leaves of Humulus scandens (family of Moraceae), fifteen compounds were isolated from the stems and leaves of H.scandens by silica gel, Sephadex LH-20, ODS, and preparative HPLC chromatography.The structures were identified by physicochemical data and spectroscopic method as tectochrysin (1), chrysin (2), 5-hydroxy-3, 4'', 6, 7-tetramethoxyflavone (3), (2S)-5-hydroxy-7, 8-dimethoxyflavanone (4), imperatorin (5), phellopterin (6), ethyl 4-hydroxy-3-(3''-methyl-2''-butenyl)benzoate (7), p-hydroxy-phenylpropionic acid (8), ethyl p-hydroxycinnamate (9), p-hydroxybenzaldehyde (10), anofinic acid (11), 5,6-dehydrokavain (12), physcion (13), olean-12-ene-3,?11-dione (14) and ergosta-4, 6, 8 (14), 22-tetraen-3-one (15), respectively.All compounds were isolated from this plant for the first time.
6.Alkaloids of Ervatamia pandacaqui
Jing XIE ; Chunlin FAN ; Jie XU ; Jian ZHANG ; Wencai YE ; Xiaoqi ZHANG
Journal of China Pharmaceutical University 2021;52(3):287-292
Eleven alkaloids were isolated from the twigs and leaves of Ervatamia pandacaqui using chromatographic methods of silica gel, Sephadex LH-20, ODS, and HPLC.Their structures were elucidated by physical,chemical and spectroscopic methods and determined as voacristine 7-hydroxyindolenine (1),iboxygaine (2), 19S-hydroxyibogamine (3), 3-oxotabersonine (4), perivine (5), pericyclivine (6), rhazinalinol (7), geissoschizol (8), 3, 14-dihydroolivacine (9), vallesamine (10), and conolobine A (11), respectively.All compounds were isolated from this plant for the first time.
7.Qualitative and quantitative analyses of Chrysanthemum morifolium ‘Fubaiju’ by LC-MSn and HPLC-UV
Junyan LI ; Thi Anh PHAM ; Zhongxuan SUN ; Xuexiang CHEN ; Wencai YE ; Hao WANG
Journal of China Pharmaceutical University 2019;50(5):565-571
A qualitative analytical method of liquid chromatography coupled with mass spectrometry(LC-MSn)was developed for the identification of main constituents in Chrysanthemum morifolium ‘Fubaiju’. High-performance liquid chromatography(HPLC)was developed for the quantification of five active components, including chlorogenic acid(1), luteolin-7-O-β-D-glucopyranoside(2), luteolin-7-O-β-D-glucopyranuronide(3), 3, 5-Di-caffeoylquinic acid(4), and apigenin-7-O-β-D-glucopyranoside(5). A total of 22 compounds, including 13 flavonoids and 9 phenolic acids, were identified based on their retention behaviors, UV profiles and MS fragment information. Furthermore, a validation method with good linearity(r> 0. 999 9), precision, stability, repeatability and recovery was successfully applied for simultaneous determination of five major components in 10 batches of C. morifolium ‘Fubaiju’ by HPLC-UV method. The established method was proved to be a validation strategy for the quality evaluation of C. morifolium ‘Fubaiju’.
8.Phenols from Vitex negundo
Ting WEN ; Jie HUANG ; Xiaojun HUANG ; Chunlin FAN ; Ying WANG ; Wencai YE
Chinese Traditional Patent Medicine 2017;39(7):1431-1434
AIM To study the phenols from Vitex negundo Linn..METHODS The ethyl acetate fraction of 70% ethanol extract from V.negundo was isolated and purified by silica,Sephadex LH-20 and ODS column,then the structures of obtained compounds were identified by spectral data.RESULTS Seven compounds were isolated and identified as luteolin-4'-O-β-D-glucopyranoside (1),isoorientin 6-O-caffeate (2),3,4,5-tricaffeoyl quinic acid (3),(+)-pinoresinol-4-O-β-D-glucoside (4),methyl isoferuloyl-7-(3,4-dihydroxyphenyl) lactate (5),benzyl 7-O-β-D-glucoside (6) and oresbiusin A (7).CONCLUSION All the compounds are isolated from this plant for the first time,and compounds 1,3,5-7 are first isolated from genus Vitex.
9.Identification of major constituents from propolis by LC-IT-TOF-MS
Jing YAO ; Jianguo SUN ; Liang WU ; Hao WANG ; Guangji WANG ; Wencai YE
Journal of China Pharmaceutical University 2017;48(2):178-183
A qualitative analytical method of liquid chromatography coupled with ion trap time-of-flight mass spectrometry (LC-IT-TOF/MS) was developed for identification of major constituents in propolis from China (Shandong).The LC-IT-TOF-MS was performed on a Shim-pack VP-ODS column (2.0 mm× 150 mm,5 μm) with the mobile phase consisting of acetonitrile and water containing 0.2% formic acid in gradient mode,and the flow rate was set at 0.3 mL/min.Negative ion mode was used for IT-TOF-MS.According to the accurate molecular weight,MS fragment pathway,comparison with the retention time of reference compounds,total 31 compounds,including twenty-five phenolic acids and six flavonoids were identified.The LC-IT-TOF-MS qualitative analysis method can be used for analyzing major components of propolis quickly and accurately.
10.Phenolic constituents of Galla Chinensis and their antiviral activities
Hanbing YANG ; Wenqiang YANG ; Min SONG ; Jian ZHANG ; Xiaoqi ZHANG ; Wencai YE
Journal of China Pharmaceutical University 2016;47(5):566-569
Seven compounds in the 95% ethanol extract of Galla Chinensis were isolated by silica gel, ODS, Toyopearl HW-40(s)and RP-HPLC. Their structures were identified on the basis of spectral data and physicochemical properties as benzoic acid, 3, 4-dihydroxy-5-[(3, 4, 5-trihydroxybenzoyl)oxy]-, 5-ethoxycarbonyl-2, 3-dihydroxyphenyl ester(1), trigallic acid(2), 1, 2, 3, 4, 6-penta-O-galloyl-β-D-glucose(3), shikimic acid(4), gallic acid(5), methyl gallate(6)and ethyl gallate(7). Among them, compound 1 was a novel compound, and compound 2 was firstly isolated from the Galla Chinensis. The inhibition tests of the constituents showed that compound 3 exhibited in vitro antiviral activity against HSV-1 and RSV A strain, RSV Long strain with IC50 values of 13. 3, 3. 3, 3. 3 mmol/L, respectively.

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